AT7867 | CAS#857531-00-1 | 1431697-86-7

AT7867
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 401100

CAS#: 857531-00-1 (free base)

Description: AT7867 is a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70S6K) and also of protein kinase A. This ATP-competitive small molecule potently inhibits both AKT and p70S6K activity at the cellular level, as measured by inhibition of GSK3beta and S6 ribosomal protein phosphorylation, and also causes growth inhibition in a range of human cancer cell lines as a single agent.

Chemical Structure

AT7867

CAS# 857531-00-1 (free base)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 401100
Name: AT7867
CAS#: 857531-00-1 (free base)
Chemical Formula: C20H20ClN3
Exact Mass: 337.13
Molecular Weight: 337.846
Elemental Analysis: C, 71.10; H, 5.97; Cl, 10.49; N, 12.44

Price and Availability

Size	Price	Availability
10mg	USD 250	2 Weeks
25mg	USD 450	2 Weeks
50mg	USD 750	2 Weeks
100mg	USD 1150	2 Weeks
200mg	USD 1850	2 Weeks
500mg	USD 3050	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: AT7867; AT 7867; AT-7867; AT7867 HCl; AT7867 dihydrochloride. AT7867 hydrochloride.

IUPAC/Chemical Name: 4-(4-(1H-pyrazol-4-yl)phenyl)-4-(4-chlorophenyl)piperidine

InChi Key: LZMOSYUFVYJEPY-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H20ClN3/c21-19-7-5-18(6-8-19)20(9-11-22-12-10-20)17-3-1-15(2-4-17)16-13-23-24-14-16/h1-8,13-14,22H,9-12H2,(H,23,24)

SMILES Code: ClC1=CC=C(C2(C3=CC=C(C4=CNN=C4)C=C3)CCNCC2)C=C1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Related: 857531-00-1 (AT7867 free base) 1431697-86-7 (AT7867 2HCl) Source: Mol Cancer Ther. 2010 May;9(5):1100-10.

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
In vitro activity:	PDX1− Ki67+ cells were rarely found in control or AT7867-treated cells, further suggesting that AT7867 may have the potential to maintain cell proliferation activity only in PPCs (Fig. S2A). Moreover, the effect of AT7867 treatment was tested on two other hESC/iPSC lines (see Materials and methods). AT7867 also induced the proliferation of PPCs differentiated from these cell lines, which suggests versatility of the small molecule (Fig. S2B and C). Reference: Stem Cell Res. 2017 Oct;24:61-68. https://pubmed.ncbi.nlm.nih.gov/28843156/
In vivo activity:	Tumor growth curve results in Fig 5A displayed that i.p. injection of AT7867 (10 and 50 mg/kg) significantly inhibited HT-29 tumor growth in nude mice. Estimated daily tumor growth results in Fig 5B further confirmed the significant anti-HT-29 tumor activity byAT7867. Notably, the mice body weight was not significantly affected by the AT7867 administration. Neither did this study notice any signs of apparent toxicities. These results, consistent with reports from other studies, suggested that the AT7867 treatment regimens here were relatively safe to the mice. IHC staining assay results in Fig 5D demonstrated that pAKT level was significantly lower in the AT7867 (50 mg/kg)-treated HT-29 tumors. Together, these results show that i.p. injection ofAT7867efficiently inhibits HT-29 tumor growth in nude mice. Reference: PLoS One. 2017 Jan 12;12(1):e0169585. https://pubmed.ncbi.nlm.nih.gov/28081222/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	28.9	85.66
	Ethanol	4.4	12.93

Preparing Stock Solutions

The following data is based on the product molecular weight 337.85 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Kimura A, Toyoda T, Nishi Y, Nasu M, Ohta A, Osafune K. Small molecule AT7867 proliferates PDX1-expressing pancreatic progenitor cells derived from human pluripotent stem cells. Stem Cell Res. 2017 Oct;24:61-68. doi: 10.1016/j.scr.2017.08.010. Epub 2017 Aug 17. PMID: 28843156. 2. Grimshaw KM, Hunter LJ, Yap TA, Heaton SP, Walton MI, Woodhead SJ, Fazal L, Reule M, Davies TG, Seavers LC, Lock V, Lyons JF, Thompson NT, Workman P, Garrett MD. AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth. Mol Cancer Ther. 2010 May;9(5):1100-10. doi: 10.1158/1535-7163.MCT-09-0986. Epub 2010 Apr 27. PMID: 20423992; PMCID: PMC4825853. 3. Zhang S, Deng Z, Yao C, Huang P, Zhang Y, Cao S, Li X. AT7867 Inhibits Human Colorectal Cancer Cells via AKT-Dependent and AKT-Independent Mechanisms. PLoS One. 2017 Jan 12;12(1):e0169585. doi: 10.1371/journal.pone.0169585. PMID: 28081222; PMCID: PMC5231330.
In vitro protocol:	1. Kimura A, Toyoda T, Nishi Y, Nasu M, Ohta A, Osafune K. Small molecule AT7867 proliferates PDX1-expressing pancreatic progenitor cells derived from human pluripotent stem cells. Stem Cell Res. 2017 Oct;24:61-68. doi: 10.1016/j.scr.2017.08.010. Epub 2017 Aug 17. PMID: 28843156. 2. Grimshaw KM, Hunter LJ, Yap TA, Heaton SP, Walton MI, Woodhead SJ, Fazal L, Reule M, Davies TG, Seavers LC, Lock V, Lyons JF, Thompson NT, Workman P, Garrett MD. AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth. Mol Cancer Ther. 2010 May;9(5):1100-10. doi: 10.1158/1535-7163.MCT-09-0986. Epub 2010 Apr 27. PMID: 20423992; PMCID: PMC4825853.
In vivo protocol:	1. Zhang S, Deng Z, Yao C, Huang P, Zhang Y, Cao S, Li X. AT7867 Inhibits Human Colorectal Cancer Cells via AKT-Dependent and AKT-Independent Mechanisms. PLoS One. 2017 Jan 12;12(1):e0169585. doi: 10.1371/journal.pone.0169585. PMID: 28081222; PMCID: PMC5231330. 2. Grimshaw KM, Hunter LJ, Yap TA, Heaton SP, Walton MI, Woodhead SJ, Fazal L, Reule M, Davies TG, Seavers LC, Lock V, Lyons JF, Thompson NT, Workman P, Garrett MD. AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth. Mol Cancer Ther. 2010 May;9(5):1100-10. doi: 10.1158/1535-7163.MCT-09-0986. Epub 2010 Apr 27. PMID: 20423992; PMCID: PMC4825853.

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1: Grimshaw KM, Hunter LJ, Yap TA, Heaton SP, Walton MI, Woodhead SJ, Fazal L, Reule M, Davies TG, Seavers LC, Lock V, Lyons JF, Thompson NT, Workman P, Garrett MD. AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth. Mol Cancer Ther. 2010 May;9(5):1100-10. Epub 2010 Apr 27. PubMed PMID: 20423992.

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